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Block 5 > Pharm - Lecture 8 - Adrenergic antagonists > Flashcards

Pharm - Lecture 8 - Adrenergic antagonists Flashcards

1
Q

What is the mechanism of adrenergic neuron blockers?

A

drugs that disrupt the synthesis, storage or release of norepinephrine

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2
Q

Which drugs are Adrenergic neuron blockers? (3)

A

1) Guanethidine
2) Guanadrel
3) Reserpine

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3
Q

What is the mechanism of Guanethidine and Guanadrel? (2)

A

Inhibits norepinephrine release and depletes neuronal amine stores

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4
Q

What is the therapeutic use of Guanethidine and Guanadrel?

A

Severe hypertension

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5
Q

What is the difference between Guanethidine and Guanadrel?

A

Guanethidine is a polar compound that does not enter the CNS

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6
Q

How are Guanethidine and Guanadrel taken up into the cell?

A

NET - therfore they are inhibited by tricyclic antidepressants that inhibit NET

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7
Q

What are the side effects of Guanethidine and Guanadrel?

A

Many side effects: orthostatic hypotension, interferes with sexual function, diarrhae, muscle weakness, edema

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8
Q

What is the mechanism of Reserpine?

A

It inhibits he vesicular monamine oxidase transporter 2 (VMAT2) therby inhibiting the synthesis of norepinephrine

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9
Q

How does Reserpine get into the cell?

A

diffusion (does not need VMAT2)

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10
Q

What is the therapeutic use of Reserpine?

A

treats essential hypertension - rarely used

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11
Q

What are the side effects of Reserpine?

A

Many CNS side effects, depression, suicide, sedation

Other side effects: diarrhae, orthostaic hypo-tension, increased gastric acid secretion

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12
Q

What is Reserpine’s length of onset and how long does it last?

A

Slow onset and Long acting

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13
Q

What is the mechanism of adrenergic receptor blockers?

A

Agents produce their major actions by inhibiting alpha and beta receptors. Both exogenously administered as well as endogenously released catecholamines are blocked

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14
Q

What drugs are alpha adrenergic receptor antoganists? (4)

A

1) Phenoxybenzamine
2) Phentolamine
3) Prazosin
4) Tamsulosin

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15
Q

Which receptors does Phenoxybenzamine and Phentolamine block?

A

a1 and a2

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16
Q

What is the mechanism of Phenoxybenzamine?

A

Irreversible antagonist via covalent bonding with receptor. New receptors need to be synthesized, so it is very long lasting

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17
Q

What is the effect of Phenoxybenzamine?

A

produces vasodilation proportional to the degree of sympathetic tone

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18
Q

What is the mechanism of phentolamine?

A

Competitive reversible antagonist

Block can be overcome by increasing the agonist

19
Q

What is the therapeutic use of Phenoxybenzamine? (2)

A

1) pheochromocytoma
2) To reverse or shorten the duration of soft-tissue anesthesia produced by combined local anesthetic and sympathomimetic

20
Q

What is the therapeutic use of Phentolamine? (3)

A

1) hypertension
2) pheochromocytoma
3) to reverse or shorten the duration of soft tissue anesthesia produced by combined local anesthetic and sympathomimetic

21
Q

What are the side effects of phenoxybenzamine and phentolamine? (2)

A

1) tachycardia and salt/water retention (edema)
2) Orthostatic hypotension

22
Q

What is the mechanism of Prazosin? How is it administered?

A

orally active - competitive blocker of a1 receptors

23
Q

What is the effect of Prazoisn?

A

1) minimal tachycardia
2) decreases vascular tone in resistance (arterioles) and capacitance (veins)
3) produce favorable lipid profile: low LDL, high HDL

24
Q

Why is reflex tachcardia less problamatic with Prazosin?

A

Prazosin doesn’t block the pre-synpatic a2 receptors very much

25
Q

What are the major therapeutic uses of Prazosin?

A

1) hypertension
2) short-term treatment of congestive heart failure (because of preload and afterload reducing agent)
3) Benign prostatic hyperplasia (BPH) - relaxes a1 mediated contraction of prostate and bladder neck that contributes to resistance to urine flow

26
Q

What are the side effects of prazosin?

A

1) “first dose” phenomenon - hypotension and syncope 30-90 minutes after first dose
2) presistent orthostatic hypotension
3) salt and water retention (edema)

27
Q

What is the mechanism and receptor selectivty for Tamsulosin?

A

a1 receptor antagonist with ome selectivity for a1A versus a1B (favors a1A receptor blockage in prostate)

28
Q

What is the therapeutic use of Tamsulosin?

A

Effective for treatement of BPH with little effect on blood pressure

Not approved for treatmenet of hypertension

29
Q

What are the non-selective beta adrenergic receptor antagonists?

A

1) Propranolol
2) Timolol
3) Metoprolol
4) Atenolol

30
Q

What is the mechanism and receptor specificty of Propranolol?

A

Competitive reversible blockade of both B1 and B2 receptors

31
Q

What are the therapeutic uses of Propanolol? (5)

A

Hypertension

Angina

cardiac arrhythmias due to excess catecholamines or that respond to a reduction in heart rate/AV conduction velocity

Acute myocardial infarction

migraine prophylaxis

32
Q

What are the side effects of Propranolol? (4)

A

Cardiac depression, bradycardia/heart block

May increase airway resistance

Mask sympoms of hypoglycemia

sedation, impotence, nightmares

33
Q

What types of patients should you be warry about giving Propranolol to? (6)

A

Patients with:

Asthma

CHF

bradyarrhythmias, AV block

insulint-dependentdiabetes prone to hypoglycemic episodes

hypotension

vasopastic angina

34
Q

What is the mechanism for Timolol?

A

Non-selective beta receptor antagonist?

35
Q

What is the therapeutic use of Timolol?

A

Similar to propranolol along with treatment of wide angle glaucoma

36
Q

What is the mechanism of Metoprolol?

A

Competitive, reversible B1 receptor blocker (low doses it is more selective at blocking the B1 receptor)

37
Q

What is the therapeutic use of metoprolol?

A

Similar to propranolol - also used to treate heart failure

38
Q

What is the mechanism of Atenolol?

A

B1 receptor antagonist

39
Q

What is the therapeutic use of Atenolol?

A

Similar to propranolol (except for migraine prophylaxis)

40
Q

What is the mechanism of Labetalol?

A

Competitive antagonist of a1 receptor and both B receptors (non-selective)

41
Q

What is the therapeutic use of Labetalol?

A

Essential hypertension and hypertensive emergencies

42
Q

What is the mechansim of Carvedilol?

A

Competitive antagonist of a1 receptor and both B receptors (non-selective)

43
Q

What is the effect of Carvedilol? (2)

A

1) anti-oxidant properties and anti-inflammatory effects
2) blocks L-type calcium channels at higher doses

44
Q

What is the therapuetic use of Carvedilol? (3)

A

1) CHF
2) Hypertension
3) Acute MI

Block 5 (23 decks)

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